Background: The generic name “flavonolignan” was created in
1968 for a relatively small class of naturally occurring hybrid molecules
biogenetically originated from ubiquitous flavonoids and lignans (phenylpropanoids).
The first group of flavonolignans was extracted from Silybum
marianum that has long been used for hepatoprotection. Recently, the medicinal
merit of flavonolignans has been extended to the prostate cancer
Methods: Systematic interpretation and summarization of the relevant literature.
Results: Over forty naturally occurring flavonolignans have so far been obtained from various
plants. Certain flavonolignans have been demonstrated by in vitro cell-based and in vivo
animal-based experiments, and human clinical studies i) to possess effective chemopreventive
function against various tumor promoters; ii) to show the anti-angiogenic efficacy; iii)
to have potential in treating prostate cancer; iv) to sensitize prostate tumors to chemotherapeutic
agents through down-regulation of P-glycoprotein and other mechanisms; and v) to
be used by prostate cancer patients to protect or treat the hepatotoxicity caused by several
chemotherapies. Certain flavonolignans can synergize with well-established chemotherapeutic
agents for prostate cancer.
Conclusion: This review provides a systematic and in-depth overview of the promise and
potential of flavonolignans in prostate cancer management, which covers their chemopreventive
effect, chemotherapeutic treatment, mechanisms of actions, synthetic derivatives,
structure-activity relationships, and the difference in inhibiting prostate cancer cell proliferation
between certain flavonoligans and their respective flavonoid counterpart. This summarization
aims to provide valuable insights into further and rational development of flavonolignans
for prostate cancer management by interpreting the data reported in the literature.